Assay Detail
Functional
CHEMBL2077530
Review assay metadata, readout intent, target linkage, and publication context from the same page.
TP_TRANSPORTER: inhibition of 9-(2-phosphonomethoxyethyl)adenine(PMEA) efflux (PMEA: 1 uM) in MRP5-expressing HEK293 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
ATP-binding cassette sub-family C member 5 (CHEMBL2046258) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Characterization of the transport of nucleoside analog drugs by the human multidrug resistance proteins MRP4 and MRP5.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 4.39 | 4.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL285913 | TREQUINSIN | 2.0 | 1 | 4.52 |
| CHEMBL932 | DIPYRIDAMOLE | 4.0 | 1 | 4.52 |
| CHEMBL15177 | MK-571 | — | 1 | 4.40 |
| CHEMBL192 | SILDENAFIL | 4.0 | 1 | 4.10 |
| CHEMBL126075 | DILAZEP | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL285913 | TREQUINSIN | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL932 | DIPYRIDAMOLE | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL15177 | MK-571 | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL192 | SILDENAFIL | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL126075 | DILAZEP | IC50 | > | 50000.0 | nM | - |